What are your colleagues reading in MedChemComm?

The articles below are some of the most read MedChemComm articles in January, February and March 2016.

Multivalent glycoconjugates as vaccines and potential drug candidates
Sumati Bhatia, Mathias Dimde and Rainer Haag
DOI: 10.1039/C4MD00143E, Review Article

Thermoresponsive fluorinated small-molecule drugs: a new concept for efficient localized chemotherapy
Catherine M. Clavel, Patrycja Nowak-Sliwinska, Emilia Păunescu and Paul J. Dyson
DOI: 10.1039/C5MD00409H, Review Article

Mechanisms of resistance to membrane-disrupting antibiotics in Gram-positive and Gram-negative bacteria
Kfir B. Steinbuch and Micha Fridman
DOI: 10.1039/C5MD00389J, Review Article

Endless resistance. Endless antibiotics?
Jed F. Fisher and Shahriar Mobashery
DOI: 10.1039/C5MD00394F, Review Article

Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
DOI: 10.1039/C4MD00216D, Review Article

Surface plasmon resonance for the characterization of bacterial polysaccharide antigens: a review
Barbara Brogioni and Francesco Berti
DOI: 10.1039/C4MD00088A, Review Article

Towards understanding cell penetration by stapled peptides
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
DOI: 10.1039/C4MD00131A, Concise Article

Rational design of protein–protein interaction inhibitors
Didier Rognan
DOI: 10.1039/C4MD00328D, Review Article

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H, Concise Article

Mechanisms of resistance to aminoglycoside antibiotics: overview and perspectives
Sylvie Garneau-Tsodikova and Kristin J. Labby
DOI: 10.1039/C5MD00344J, Review Article

Read more »

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Dr Alessio Ciulli wins 2016 Emerging Investigator Lectureship

Dr Alessio Ciulli winner of the 2016 MedChemComm Emerging Investigator LectureshipCongratulations to Dr Alessio Ciulli from University of Dundee, UK, the recipient of the 2016 MedChemComm Emerging Investigator Lectureship.

The annual MedChemComm Emerging Investigator Lectureship is given to a researcher who has made a significant contribution to medicinal chemistry research in the early part of their career.

The Editorial Board have selected Dr Alessio Ciulli as this year’s recipient for his work tackling important biology with elegant chemistry; developing novel chemical tools to aid our understanding of BET bromodomain proteins and providing pioneering examples of understanding protein-protein interactions as a basis for discovering novel therapeutics.

On being told he had won Dr Ciulli said,

I feel truly honoured to have been selected to receive the MedChemComm Emerging Investigator Lectureship this year, and privileged to join such a distinguished list of former winners. It is a recognition to the excellent work of many students and postdocs in my group who have made key contributions to our discoveries over the past few years. I am excited to be given the opportunity to present some of our latest results at a conference later in the year.”

Alessio will be presenting his lectureship at this year’s EFMC International Symposium on Medicinal Chemistry in Manchester. Register now.

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Updated guidelines and standards for MedChemComm

We’re about to publish our first new issue of 2016 and with it come some changes to the journal which we hope will enhance MedChemComm for our readers, authors and reviewers.

More detailed scope and significance guidelines
We’ve updated our scope and significance guidelines to provide more detail about the type of research we publish, to help authors decide if MedChemComm is the right journal for their article. Also we now ask authors to provide a very brief statement on submission of their article which describes why their research is a significant advance in their field. This information assists our editors and referees in assessing the article’s suitability for publication in the journal.

Introducing ‘Research Articles’
Primary research articles in MedChemComm, which were previously called ‘Concise Articles’, are now ‘Research Articles’. There’s no change in the length or style of articles; ‘Research Articles’ can accommodate any type of primary research article, including communication and full paper styles. The change in name is purely to better reflect this breadth of style. You’ll start seeing the new article name from issue 2 this year.

Article layout
One of the most important aspects of an article from a reader’s point of view is that it’s easy to find and read, with the key information readily available. Therefore we’ve updated guidelines on writing titles and abstracts, which gives advice on how to make these as impactful as possible. This is something we’ll now ask referees to comment on when assessing a manuscript. Also we’ll be limiting the amount of experimental detail included in the main text to two journal pages. Authors should still provide as much experimental information and data as is required for their research; however anything over the two pages should be included in the supplementary information rather than the main text.

Experimental information and data
It’s important that the research published in MedChemComm has the highest levels of integrity and reproducibility; therefore we’ve updated our guidelines on experimental information and data. These give authors information on how much experimental detail should be included, what data are required and the format in which they should be presented.

Feel free to send us any comments or suggestions about these changes or anything else to do with the journal. Thank you to all our authors, reviewers and readers for your continued support, and I hope you enjoy reading MedChemComm in 2016.

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2016 MedChemComm Emerging Investigator Lectureship – Nominations open

The launch of the 2016 MedChemComm Emerging Investigator Lectureship. Who will you nominate?

We are pleased to announce that nominations for the 2016 MedChemComm Emerging Investigator Lectureship are now open and we are looking for your suggestions.

Nominations will close 22nd January 2016.

The recipient will receive a contribution of up to £1000 towards speaking at a conference of their choice.

Qualification
The lectureship is open to candidates who received their PhD on or after December 31st 2005 and who have made a significant contribution to medicinal chemistry in their early career, particularly if they have brought new ideas to drug discovery.

How to nominate
If you would like to nominate someone please email us (medchemcomm-rsc@rsc.org) with the following:

  • Their name
  • Their affiliation
  • At least one paragraph explaining their achievements and why they should be considered

Additional supporting information, for example their CV, would be very much appreciated but is not mandatory for making a nomination.

Self-nominations are accepted but must be supported by a letter of support from your Head of Departments or similar person at your institute.

Selection
The decision to award the lectureship will be made by a panel of MedChemComm Editorial Board members.

Previous Lectureship winners include:

  • Professor Richard Payne (University of Sydney, Australia)
  • Professor Patrick Gunning (University of Toronto, Canada)
  • Professor Christian Heinis (École Polytechnique Fédérale de Lausanne, Switzerland).
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What are your colleagues reading in MedChemComm?

The articles below are the most read MedChemComm articles in July, August and September 2015.

Transition metal diamine complexes with antimicrobial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA)
G. W. Karpin, D. M. Morris, M. T. Ngo, J. S. Merola and J. O. Falkinham III
DOI: 10.1039/C5MD00228A, Concise Article

Multivalent glycoconjugates as vaccines and potential drug candidates
Sumati Bhatia, Mathias Dimde and Rainer Haag
DOI: 10.1039/C4MD00143E, Review Article

Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects
Isidro Cortés-Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke B. Lenselink, Oscar Méndez-Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prusis, Thérèse E. Malliavin, Gerard J. P. van Westen and Andreas Bender
DOI: 10.1039/C4MD00216D, Review Article

Towards understanding cell penetration by stapled peptides
Qian Chu, Raymond E. Moellering, Gerard J. Hilinski, Young-Woo Kim, Tom N. Grossmann, Johannes T.-H. Yeh and Gregory L. Verdine
DOI: 10.1039/C4MD00131A, Concise Article

Rational design of protein–protein interaction inhibitors
Didier Rognan
DOI: 10.1039/C4MD00328D, Review Article

Magic molecule modifiers
Derek Lowe
DOI: 10.1039/C5MD90028J, In the Pipeline

Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor
Katherine S. England, Anthony Tumber, Tobias Krojer, Giuseppe Scozzafava, Stanley S. Ng, Michelle Daniel, Aleksandra Szykowska, KaHing Che, Frank von Delft, Nicola A. Burgess-Brown, Akane Kawamura, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C4MD00291A, Concise Article

Identification of an inhibitor of the ubiquitin–proteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
Caroline Haglund, Chitralekha Mohanty, Mårten Fryknäs, Padraig D’Arcy, Rolf Larsson, Stig Linder and Linda Rickardson
DOI: 10.1039/C3MD00386H, Concise Article

Amphiphilic designer nano-carriers for controlled release: from drug delivery to diagnostics
Malinda Salim, Hiroyuki Minamikawa, Akihiko Sugimura and Rauzah Hashim
DOI: 10.1039/C4MD00085D, Review Article

Design and synthesis of potent and selective inhibitors of BRD7 and BRD9 bromodomains
Duncan A. Hay, Catherine M. Rogers, Oleg Fedorov, Cynthia Tallant, Sarah Martin, Octovia P. Monteiro, Susanne Müller, Stefan Knapp, Christopher J. Schofield and Paul E. Brennan
DOI: 10.1039/C5MD00152H, Concise Article

Read more »

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2016 RSC Prizes and Awards in Organic Chemistry & Chemical Biology now open for nomination

Nominate someone you know who is an exceptional talent in chemical sciences

The 2016 RSC Prizes and Awards are now open for nomination!

Nominations will close on 15 January 2016.


For more than 140 years, our Prizes and Awards programme has been acknowledging and celebrating exceptional talent in the chemical sciences, and with your support we are hoping that 2016 will even more successful!

Last year’s winners include Chemists such as Prof. Wilfred van der Donk (University of Illinois), Prof. Tim Donohoe (University of Oxford), Prof. Shuli You (Shanghai Institute of Organic Chemistry), Prof. Philip Gale (University of Southampton), Prof. Herman Overkleeft (Leiden University), Prof. Alison Ashcroft and Prof. Sheena Radford (University of Leeds).

This year we have 63 prizes and awards open for nominations of individuals, teams and organisations covering the breadth of the chemical sciences across academia, education and industry.

This year’s prizes in the field of Organic Chemistry & Chemical Biology include:

CBID (Chemistry Biology Interface Division) awards –

Organic Awards –

For 2016 our Longstaff Prize is also open – since 1881 we have awarded this prize once every three years to one of our members who has achieved the most to advance the science of chemistry.

Submit your suggestions now!

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Poster Prize Winners at EuCheMS Conference

Congratulations to the Poster Prize winners at the 6th EuCheMS Conference on Nitrogen Ligands!

The winners are:

Sophie Laine (MedChemComm) – “Potential MRI Contrast Agent for Enzymatic Detection”

Neeladri Das (Chemical Science) – “Pyrazinc Based Tectons in the Self-Assembly of Finite Two­ Dimensional Supramolecular  Ensembles”

Nicole Kindermann (Dalton Transactions) – “A dicopper pyrazole/tacn system and its diOX) gcn chemistry”

Florian Schendzielorz (Dalton Transactions) – “A Well Characterized Osmium(IV)-Nitrido  Complex in a Square­ Planar  Coordination Geometry”

Charles Lochenie (Dalton Transactions) – “Synergetic effects between spin state change and fluorescent properties of Schiff base-like 3d metal complexes”

Amandine Conte-Daban (Inorganic Chemistry Frontiers) – “A new probe to determine the affini ty constant of Cu 2+ for A”

Yasin Kuzu (Inorganic Chemistry Frontiers) – “Planar ChiraJ 2-(N ,N-Dimethylaminomethyl)-1-(trimethyl­silyl)ferrocenyl Substitu ted Silanols,Silanolates and Siloxanes”

Maxim A Faraonov (Materials Horizons) – “Crystalline Salts with Radical Anions of Metal-containing and Metal­ free Pbthalocya nincs:Synthesis, Crystal Structures, Optical and Magnetic Properties”

The conference was held from 13th – 17th September in Beaune, France.  The conference aims to attract scientists with an interest in the field of metal-nitrogen ligand chemistry.  This year it also included these topics: the recent advances in the fields of coordination chemistry, metal-organic chemistry, bioinorganic chemistry, and materials & catalysis.

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Phenotypic Drug Discovery Web Themed Issue

MedChemComm is delighted to announce a high-profile themed issue on Phenotypic Drug Discovery, due for publication online in mid-2016. The issue is being Guest Edited by Dr Fabien Vincent (Pfizer), Dr Jonathan A. Lee (Eli Lilly) and Professor Michael Pollastri (Northeastern University).

Deadline for Submission: February 1, 2016

The level of quality of this issue will be high, and all manuscripts will subject to the journal’s normal standards and peer review process. Guidelines are available at rsc.li/1K0EgYx and rsc.li/1JAwCbA

If you are interested in taking part in this issue, please email MedChemComm: medchemcomm-rsc@rsc.org

Scope of the issue

Phenotypic approaches are highly complementary to the molecular target centric strategy that prevails in Pharma and moreover, may mitigate future clinical failure issues related to target validation and lack of efficacy. Five years into the Phenotypic Drug Discovery (PDD) Renaissance, this issue aims to shift the main focus in this area from assays and screens towards the medicinal chemistry programs engendered by these early efforts. Manuscripts covering the lessons learned and progress recorded on the road to clinical candidates in the areas highlighted below are actively sought:

  • Design of compound libraries for phenotypic screening (e.g. biologically annotated, diversity-based and natural products libraries)
  • Identification of novel targets for disease-relevant phenotypes
  • Identification of novel chemical matter or molecular mechanisms of action for known molecular targets
  • Identification of novel cellular roles for known targets
  • Challenges in PDD hit triage such as compound/series prioritization and validation
  • Challenges in driving an SAR  using complex assay systems (in vitro and in vivo systems)
  • Safety derisking and compound/project progression in the absence of a known target
  • Chemical biology approaches for mechanism and target deconvolution

New research in MedChemComm is published as Concise Articles. This article type encompasses both Communication and Full Paper styles with no strict page limit. There is also the opportunity to write a Review article for the issue, and if you would be interested in this please let us know.

MedChemComm is the Royal Society of Chemistry journal covering all areas of medicinal chemistry research, including research that interfaces with other areas of the chemical sciences, biology, materials science or physics

The journal is in partnership with the European Federation for Medicinal Chemistry (EFMC), and the co-Editors-in-Chief are Dr. Tony Wood (Pfizer) and Professor Greg Verdine (Harvard University). To view recent articles or to find out more about the journal please visit the website at www.rsc.org/medchemcomm

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Membrane Transporters: Solute Carriers themed issue launched

MedChemComm is delighted to announce a high-profile themed issue on Membrane Transporters, focussing on solute carriers (SLCs). The Guest Editors for this issue are Professor Matthias A. Hediger (University of Bern, Switzerland) and Dr David Hepworth (Pfizer, Cambridge, USA).

Deadline for Submission: December 14 2015

Please e-mail the Editorial Office if you are interested in contributing an article.

Manuscripts can be submitted using the Royal Society of Chemistry’s online article submission service. Please clearly state that the manuscript is submitted for the themed issue on Membrane Transporters: Solute Carriers.

The level of quality of this issue will be high, and all manuscripts will undergo the journal’s normal peer review process.

Scope

Metabolic homeostasis within cells requires strict control over the import and export of metabolites, nutrients and ions across membranes. Polar chemical species such as these have negligible ability to cross phospholipid membranes by simple diffusion and instead require highly regulated transport proteins to control their movement. The largest class of transport proteins is the solute carrier series (www.bioparadigms.org) and it is on this superfamily that this special issue of MedChemComm will focus.

These proteins are of great interest for basic academic research, but beyond that they are of central importance in a number of areas of applied science: as drug targets, as controllers of drug disposition and pharmacokinetics, and as the cause of drug toxicity.

Known SLC drug targets include:

  • The monoamine transporter family which contains the serotonin transporter (SLC6A4) target of the highly important SSRI drug class
  • SLC5A2 (SGLT2), an important new anti-diabetic target to block renal glucose reabsorption
  • Sodium chloride transporters (SLC12 family) – the targets of loop and thiazide diuretics

SLCs important in drug pharmacokinetics and disposition include

  • The OATP (SLCO) and OAT (SLC22) family  of anion transport
  • The OCT (SLC22) family of cation transport
  • The SLC47 multidrug and toxin extrusion family

SLCs important in drug toxicity include the thiamine transporter SLC19A2

All areas of research where the chemical sciences have impacted the study of the SLC superfamily will be considered for inclusion in this themed issue. Examples include, but are not limited to:

  • Medicinal chemistry and molecular probe design against these target families
  • Chemical biology approaches to allow for detailed study of these protein classes including physiological roles, disease mechanisms, etc.
  • Structural biology and biophysics of integral membrane proteins as relevant to ligand design and/or chemical biology
  • Molecular modelling that has enabled drug and probe design
  • The impact of transporters on drug disposition and pharmacokinetics – with a particular interest in structure activity relationships for such transport
  • The study of toxins and venoms which act through these target classes
  • Novel screening methodologies that allow the identification of new inhibitors, modulators and substrates of this protein class
  • The application of new cell biology techniques such as gene-editing, silencing and haploid genetic approaches that allow the study of chemical agents acting via these target families
  • Systems biology approaches to the study of chemical modulators and substrates of membrane transport proteins

The issue will consist of a series of research articles and reviews from prominent scientists who are committed to applying excellence in ion channels and membrane transporter research toward the treatment of human diseases, combining breakthroughs in both basic science and applied science, such as drug discovery.

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2015 Emerging Investigator Lectureship

Professor Richard Payne to present his lecturre at Chemical Protein Synthesis Meeting

Earlier this year Professor Richard Payne from University of Sydney, Australia, was announced as the the recipient of the 2015 MedChemComm Emerging Investigator Lectureship.

We are pleased to let you know that Richard will be presenting his talk entilted:

New ligation technologies for the rapid assembly of modified proteins

at the upcoming Chemical Protein Synthesis (CPS) Meeting in St. Augustine, Florida on Friday the 19th of June.

The meeting starts on the 16th of June  2015 and online registration for the meeting closes the 10th of June – so there’s still time to register to see Richard’s talk!


UPDATE: Prof. Payne’s talk was very well received at the successful Chemical Protein Synthesis Meeting, where he (left) was presented his lectureship by Professor Stephen Kent (right).

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